SR 16832
Based on 1 Customer Validation
SR 16832 is a dual-site covalent, orthosteric and allosteric PPARγ antagonist. SR 16832 activates the TGF-β signaling pathway and upregulates the expression of Vimentin and Fibronectin (Fibronectin). SR 16832 is toxic to bronchial epithelium. SR 16832 can be used in research related to type 2 diabetes and pulmonary fibrosis.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.58%
- CAS 番号: 2088135-12-8
- 分子式: C17H12ClN3O4
- 分子量:357.75
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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PPARγ |
SR 16832 (5 μM MRL20 post-treatment) completely inhibits allosteric cellular activation of Gal4-PPARγ LBD by MRL20 in HEK293T cells, while having minimal impact on basal Gal4-PPARγ LBD activity[1].
SR 16832 lowers basal transactivation of full-length PPARγ and completely inhibits allosteric cellular activation of full-length PPARγ by MRL20 in HEK293T cells[1].
SR 16832 weakens the allosteric potency of MRL20 to recruit TRAP220 coactivator peptide to purified PPARγ LBD, including in the presence of RXRα LBD[1].
SR 16832 completely blocks allosteric binding of rosiglitazone to purified PPARγ LBD, preventing TRAP220 coactivator peptide recruitment[1].
SR 16832 weakens the allosteric potency of MRL20 to modulate NCoR corepressor peptide binding to purified PPARγ LBD[1].
SR 16832 completely inhibits allosteric cellular activation of Gal4-PPARγ LBD by Rosiglitazone (HY-17386) in HEK293T cells[1].
SR 16832 (1, 2, ..., 200 μM) exhibits cytotoxicity in human bronchial epithelial BEAS-2B cells with an EC20 of 5 μM[2].
SR 16832 (5 μM; 4, 24, and 72 h) activates TGF-β signaling, increases inflammation, and upregulates vimentin and fibronectin expression in human bronchial epithelial BEAS-2B cells[2].
SR 16832 (10 μM; 4, 24, and 72 h) activates TGF-β signaling, increases inflammation, and upregulates vimentin and fibronectin expression in primary normal human bronchial epithelial (NHBE) cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human bronchial epithelial BEAS-2B cells
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Concentration:5 μM
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Incubation Time:4 h, 24 h, 72 h
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Result:Increased TGF-β expression 2-fold relative to control at 4 h (p < 0.01).
Increased TNF-α expression 1.5-fold relative to control at 24 h (p < 0.01).
Increased vimentin expression 3-fold relative to control at 24 h (p < 0.001).
Increased fibronectin expression 3.5-fold relative to control at 72 h (p < 0.001).
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Cell Line:primary normal human bronchial epithelial (NHBE) cells
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Concentration:10 μM
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Incubation Time:4 h, 24 h, 72 h
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Result:Increased TGF-β expression 4-fold relative to control at 4 h (p < 0.001).
Increased TNF-α expression 1.5-fold relative to control at 24 h (p < 0.01).
Increased vimentin expression 3.5-fold relative to control at 24 h (p < 0.01).
Increased fibronectin expression 4.5-fold relative to control at 72 h (p < 0.001).
化学情報
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CAS 番号 2088135-12-8
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性状 Solid
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分子量 357.75
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分子式 C17H12ClN3O4
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Color White to off-white
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SMILES
O=C(NC1=CC=NC2=CC=C(OC)C=C12)C3=CC([N+]([O-])=O)=CC=C3Cl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 250 mg/mL (698.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (278 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Brust R, et al. Modification of the Orthosteric PPARγ Covalent Antagonist Scaffold Yields an Improved Dual-Site Allosteric Inhibitor. ACS Chem Biol. 2017;12(4):969-978. [Content Brief]
[2]. Jeong J, et al. Advancing the Adverse Outcome Pathway for PPARγ Inactivation Leading to Pulmonary Fibrosis Using Bradford-Hill Consideration and the Comparative Toxicogenomics Database. Chem Res Toxicol. 2022 Feb 21;35(2):233-243. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7952 mL | 13.9762 mL | 27.9525 mL | 69.8812 mL |
| 5 mM | 0.5590 mL | 2.7952 mL | 5.5905 mL | 13.9762 mL | |
| 10 mM | 0.2795 mL | 1.3976 mL | 2.7952 mL | 6.9881 mL | |
| 15 mM | 0.1863 mL | 0.9317 mL | 1.8635 mL | 4.6587 mL | |
| 20 mM | 0.1398 mL | 0.6988 mL | 1.3976 mL | 3.4941 mL | |
| 25 mM | 0.1118 mL | 0.5590 mL | 1.1181 mL | 2.7952 mL | |
| 30 mM | 0.0932 mL | 0.4659 mL | 0.9317 mL | 2.3294 mL | |
| 40 mM | 0.0699 mL | 0.3494 mL | 0.6988 mL | 1.7470 mL | |
| 50 mM | 0.0559 mL | 0.2795 mL | 0.5590 mL | 1.3976 mL | |
| 60 mM | 0.0466 mL | 0.2329 mL | 0.4659 mL | 1.1647 mL | |
| 80 mM | 0.0349 mL | 0.1747 mL | 0.3494 mL | 0.8735 mL | |
| 100 mM | 0.0280 mL | 0.1398 mL | 0.2795 mL | 0.6988 mL |
SR 16832 関連分類
HY-112247 関連分類
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